ISSN (Print): 1568-0266
ISSN (Online): 1873-4294
Volume 18, 32 Issues, 2018
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ISSN (Print): 1568-0266
ISSN (Online): 1873-4294
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Special Issue Submission
Selected Heterocyclic Compounds as Antioxidants. Synthesis and Biological Evaluation, 2014 :14(22); 2462 - 2477
E. Tsolaki, P. Nobelos, A. Geronikaki and E.A. Rekka
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Submit Abstract via Email
It has been a wonderful experience publishing our research paper with Bentham Science Publishers, who is very prompt and professional in providing excellent services. Due to this very reason, I would like to publish my forthcoming research results in the Bentham Science Publication “Current Topics in Medicinal Chemistry”.
S.K Srivastava (The Medicinal Chemistry Department, CSIR-CIMAP, Lucknow (U.P), , India)
Has contributed: QSAR Guided Semi-synthesis and In-Vitro Validation of Anticancer Activity in Ursolic Acid Derivatives
6 Abstract Ahead of Print are available electronically
19 Ahead of Print article(s) are available electronically
Cyclic peptides and peptidomimetic molecules (modified peptides) play
critical roles in natural processes, and can also be synthesized for use as research
tools and therapeutics. Protein-Protein Interactions (PPIs) play central
roles in regulating almost all biological processes across organisms and the
central dogma of biology. Compared to small molecules and antibodies, peptides
are advantageous for targeting PPIs because they maintain conformational
flexibility, can be synthesized using relatively straightforward techniques
and are generally less expensive. However, linear peptides are limited
by poor stability and inefficient cell membrane permeability. On the other
hand, cyclic peptides offer improved metabolic stability, bioavailability and
selectivity compared to their linear counterparts; moreover, cyclic peptides are particularly useful for targeting PPIs because
they maintain these enhanced drug-like properties without compromising bioavailability, as often occurs with linear peptides.
Thus, the development of cyclic peptides and peptidomimetics is of great interest in medicinal chemistry, as evidenced by numerous
investigational and approved cyclic peptide pharmaceutical compounds.
This thematic issue is comprised of six strong papers authored by esteemed colleagues renowned for their work in the field
of medicinal chemistry. The overarching topics covered include cyclic peptides in natural and therapeutic settings, the design of
cyclic peptides, several approaches to synthesize cyclic peptides, and examples of cyclic peptides in biological systems. First,
Rubin and Qvit present the first comprehensive review, analysis and critique of backbone-cyclized peptides, discussing their
design, construction, development, and application. To address the construction of backbone-cyclized peptides, Rubin, Tal-
Gan, Gilon, and Qvit subsequently provide a detailed guide for the conversion of protein active regions into peptidomimetic
therapeutic leads – delineating the identification of PPI sites, the definition of bioactive pharmacophores and the use of backbone
cyclization and cycloscan techniques to develop lead compounds.
Next, Perez reviews additional approaches for design of peptidomimetics and discusses their core properties, while comparing
and contrasting the medicinal chemistry and biophysical approaches for discovery and development. Testa, Papini, Chorev
and Rovero extensively discuss approaches to synthesize cyclic peptides and peptidomimetics, including in depth analysis of
the chemistries required to perform ring closing metathesis, lactamization, copper-catalyzed azide alkyne cycloaddition, and
other cyclization reactions. Following this, Hillman, Nadraws and Bertucci delve into stapled peptides and focus on recent advances
in their use for targeting PPIs therapeutically.
Lastly, Mull, Harrington, Sanchez, and Tal-Gan present examples of cyclic peptides in biological systems through an analysis
of cyclic peptide scaffolds in signal transduction pathways across a spectrum of prokaryotic and eukaryotic organisms as
models for the discovery of novel and broadly applicable therapeutic lead compounds.
It was an honor to compile this timely issue. Thanks to the journal for providing the opportunity for our colleagues and us to
share our perspectives. We hope the readers find this material engaging and useful, and that it will inspire further inquiry and
Cancer metabolism is an emerging area of research that offers an opportunity to target specific
metabolic vulnerabilities of cancer cells. Cancer cells undergo oncogene-mediated metabolic
reprogramming in order to meet their energy demands. Cancer cells adapt to their
microenvironment and rewire their metabolism to rely heavily on anaerobic glycolysis, a
phenomenon known as the ’Warburg effect’. In addition, cancer cells get addicted to glutamine and also
up regulate fatty acid synthesis to support their survival and rapid proliferation. Recently, there has
been a resurgence of interest in targeting carbohydrate, amino acid, and fatty acid metabolic pathways for
treatment of cancer and overcoming drug resistance in chemotherapy. Other emerging concepts include
targeting mitochondrial metabolism for the treatment of cancer. The overarching theme of this issue is to
highlight the current application, advances, and emerging concepts in the field of cancer metabolism and
discuss the prospects of metabolic inhibitors as next generation cancer therapeutics. The issue will also
emphasize medicinal chemistry efforts aimed at developing small molecule inhibitors targeting aberrant
No Text Found
The term "alternative" is employed to describe the test method in association with the principles of
the 3Rs - Replacement, Reduction and Refinement. In accordance with this principle, an alternative
method can be used to replace animal testing, reduce the quantity of animals required for each assay,
or refine an animal testing method to minimize pain and suffering.
There are different platforms available to create alternative methods including in vitro models and
computer-based systems. A few elements may be considered in terms of safety when it comes to the
development of a new drug or biomaterial. First it is important to identify the chemical identity and
the composition, as well as chemical structure, impurities and functional groups, followed by the determination
of the physical chemical properties. As a next step, the kinetics aspects, e.g. absorption,
distribution, metabolism and excretion should be evaluated. The mode and /or mechanism of action or
adverse outcome pathways as well as the chemical and biological interaction must be determined. Finally, the responses found
in alternative assays can lead to a proper safety assessment for drugs and biomaterials without the need for animal experimentation.
Within this context, this thematic issue focused on alternative assays applied to replace animal testing in order to assess the
safety and biological activity of currently available and novel drugs and biomedical devices. The manuscript entitled "Epithelial
organotypic cultures: a viable method to address the mechanisms of carcinogenesis by epitheliotropic viruses" describes the
mechanism of carcinogenesis, a topic that was initially researched mainly in animal models.
In another context, some alternative methods have also been employed in biomaterials, as the authors of “Current Methods
Applied to Biomaterials – Characterization Approaches, Safety Assessment and Biological International Standards” extensively
described. This review shows that using alternative tests for biomaterials has almost replaced animal tests, following an actual
tendency. Finally, the last two manuscripts, “Validation cytotoxicity assay for lipophilic substances” and “Alternative methods
to animal studies for the evaluation of topical/transdermal drug delivery systems” are important both for medicine and cosmetics
formulation, as the authors showed the importance to characterize the lipophilic substances, even a difficult issue in cytotoxicity
assays, and the importance of permeation in cosmetics and medical products.
Overall this special issue has addressed aspects concerning alternative assays applied to replace animal testing in order to
assess the safety and biological activity of currently available and novel drugs and biomedical devices and contain materials
that follow the topics in trends and published worldwide. This issue shows balanced viewpoints of experts contributing to
minimize the use of animal tests, in an attempt to act as a primary reference for industrial, commercial and research perspective
in an extensive field of science.
Head and neck squamous carcinoma (HNSCC) is the sixth most common malignant cancer in the world and it is characterized
by a poor prognosis. In fact, the estimated survival rate is 5 years from diagnosis.
The prognosis of the disease is significantly related to the stage in which the disease is diagnosed. Moreover, the therapies
are too invasive and not very efficient, disfiguring and debilitating the survivor’s quality of life which is much compromised.
Nowadays, there is not a reliable and non-invasive method for early diagnosis of oral squamous cell carcinoma and the simple
visual examination of the oral cavity is characterized by low sensitivity and specificity, also because the early stages of oral
carcinogenesis are not associated with clear clinical abnormalities in a significant number of patients.
The current issue of “Current Topics in Medicinal Chemistry (CTMC)” is aimed at reviewing the actual knowledge regarding
the HNSCC in order to cover this field with a broad series of papers. The first review was prepared by an Italian team led
by Fatima Ardito, Giovanni Di Gioia, Mario Roberto Pellegrino and Lorenzo Lo Muzio. The authors describe the role of genistein
as a potential anticancer agent against HNSCC. The second contribution is from Linda L. Eastham, Candace M. Howard,
Premalatha Balachandran, David S. Pasco, and Pier Paolo Claudio. In this case, the authors review the role of dietary phytochemicals
as an alternative approach to prevent HNSCC. The third review, led by Riccardo Concu and Maria Natalia Dias-
Soeiro Cordeiro, deals with the role of the Cetuximab in the treatment of HNSCC. The fourth contribution concerns the Aurora
kinase inhibitors in head and neck cancer; this work was prepared by a Chinese-Japanese team led by Guangying Qi, Jing Liu,
Sisi Mi, Takaaki Tsunematsu, Shengjian Jin, Wenhua Shao, Tian Liu, Naozumi Ishimaru, Bo Tang and Yasusei Kudo. Moving
on, Nicola Sgaramella and Karin Nylander review covers the topic of searching for new targets and treatments in the battle
against squamous cell carcinoma of the head and neck. Concu and Cordeiro present an innovative paper dealing with the development
of a new QSAR model aimed at the identification of new inhibitors for the epidermal growth factor receptor. Finally,
Ardito et al. present a new in vitro study of the inhibition activity of the curcumin against squamous cell carcinoma of tongue.